6-(2-Phenylethyl)nicotine: A novel nicotinic cholinergic receptor ligand

被引：4
|
作者：
Ramunno, A
Dukat, M
Lee, M
Young, R
El-Zahabi, M
Damaj, MI
Martin, B
Glennon, RA
机构：
[1] Virginia Commonwealth Univ, Dept Med Chem, Sch Pharm, Richmond, VA 23298 USA
[2] Virginia Commonwealth Univ, Dept Pharmacol & Toxicol, Sch Med, Richmond, VA 23298 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 13期
关键词：
nACh receptors; antagonist;
D O I：
10.1016/j.bmcl.2005.04.072
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
6-(2-Phenylethyl)nicotine (1b; K-i = 15 nM) was unexpectedly found to bind at alpha 4 beta 2 nicotinic cholinergic (nACh) receptors. Although this compound failed to produce nicotine-like agonist action in several functional assays, 1b antagonized the antinociceptive effects of nicotine (mouse tail-flick assay) in a dose-dependent fashion when administered via an intrathecal route. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码：3237 / 3240
页数：4
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